Common abnormalities that drive the growth of cancer cells are mutations in enzymes known as kinases. Several drugs that target these enzymes are already on the market as effective anti-cancer therapies and many more are in development. In addition, there have been significant improvements in the ability to synthesize specific kinase inhibitors. However, there remains a major need to understand the structural basis of compound selectivity, prospectively identify patients likely to respond to a kinase inhibitor, design improved pharmacodynamic endpoints, and understand the molecular basis of resistance to kinase inhibitor therapy. The purpose of this meeting is to discuss the lessons learned from the clinical trials of these drugs to assist in the efficient development of new drugs of this class entering or in clinical trials. By facilitating the development of these drugs, we hope to improve the outcome for patients with cancer as rapidly as possible.